Term
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Definition
development and maintenance of female reproductive tissues- uterus and breast
pregnancy
other tissues-brain, other(?) |
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Term
| hormonal regulation of the reproductive cycle-menstruation (days 1-5) |
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Definition
| declining E and P levels lead to increased prostaglandins, decreased blood flow to endometrium, and death and loss of tissues |
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Term
| hormonal regulation of the reproductive cycle-preovulation/proliferative (days 6-14) |
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Definition
one follicle dominates, produce E in response to LH (associated with slight rise in FSH)
LH spike occurs (in response to increase in E?), leads to rupture of follicle and release of ovum |
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Term
| hormonal regulation of the reproductive cycle-postovulatory/secretory (days15-28) |
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Definition
| LH spike simulates ruptured follicle to become corpus luteum, which releases P (major) and E (minor). corpus luteum has limited lifespan (14 days) |
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Term
| hormonal regulation of the reproductive cycle- if ovum IS fertilized |
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Definition
| fertilized egg/embryo secretes human chorionic gonadotropin (hCG). hCG acts like LH to stimulate corpus luteum and enhance P levels. Higher P levels support maintenance of endometrium-proper environment for embryonic development |
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Term
| hormonal regulation of the reproductive cycle -if ovum is NOT fertilized |
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Definition
| corpus luteum becomes corpus albicans, decreasing E and P levels. Lack of feedback repression by P and E on hypothalamus and anterior pituitary leads to GnRH and FSH rise. deceasing E and P lead to loss of endometrium |
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Term
| steroid contraceptive objectives |
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Definition
1. inhibit pituitary function to prevent ovulation through negative feedback mechanisms
2. shrink ovaries through inhibition of follicular development
3. alter uterus morphology to make implantation an unlikely event
4. avoid side effects of prolonged hormone treatment |
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Term
| challenges to progestin drug development |
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Definition
receptor selectivity and duration
target only necessary receptors and lengthen duration to attain better compliance
BIG CONCERN: bloating, hypertension, nausea
therapeutic considerations: contraception-no cross-reactivity with androgen or estrogen receptor. if taken with estrogens, also would prefer slight anti-mineralocorticoid activity, low number of doses, taken orally |
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Term
| key therapeutic goals for progestins in OC's |
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Definition
block androgenic effects
block bloating/water retention (associated with MR binding of progestins AND estrogen induction of aldosterone synthesis) |
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Term
| mechanism of contraceptive action- estrogen and progestin combinations |
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Definition
1. inhibition of GnRH release
2. suppress the response of pituitary gonadotropins to GnRH
3. prevent ovulation-prevent follicular growth and the emergence of a dominant follicle
4. endometrial and cervical secretion changes caused by the progestin (later) |
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Term
| starting oral controceptives- combination therapy (E and P) |
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Definition
advantages: prevents ovulation, very low failure rate
disadvantages: some adverse effects in women (nausea, bloating, high blood pressure, breast tenderness) |
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Term
| starting oral controceptives- progestin only ("minipill") |
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Definition
advantages: no estrogen adverse effects
disadvantages: does not prevent ovulation, failure rate increases greatly with missed dose |
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Term
| Four major types of combination therapy strategies depending on the different kinds of doses |
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Definition
monophasic: Brevicon, Yaz
biphasic: Neocon
triphasic: Enpresse, Ortho-Tri-Cyclen
quadraphasic: Natazia |
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Term
| advantages to multiphasic |
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Definition
minimize total steroid dose/cycle
maximizing contraceptive effect |
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Term
| disadvantages to multiphasic |
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Definition
more expensive than monophasic
more difficult to follow and adjust to missed doses
increased risk for thrombotic events with newer progestins |
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Term
| Progestin only ("minipill") |
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Definition
no estrogen
all tablets contain the same dose of progestin
brand(progestin): Micronor (norethindrone), Nor-QD (norethindrone), Overette(norgestrel)
28 tablets- all active
problems with progestin only pills: failure rate somewhat higher than combination OC's, frequent menstrual irregularities |
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Term
| monophasic combination therapy |
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Definition
same amount of E and P
21 day cycle tablets: wait 7 days after each cycle is finished before starting again
28 day cycle tablets: tablet taken each day (7 inert pills), sometimes inert pills are iron supplements to minimize anemia during withdrawal bleeding |
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Term
| removing the "inert" week |
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Definition
-most OCs have a 7 day inert period: allows for normal timing of bleeding and increases compliance with daily pill and assures patient that she is not pregnant
recent studies prove inert week is not always necessary: patient can stay on monophasic combination regimen to 6-12 weeks, followed by 1 week of inert pills, Seasonale, Seasonique, Lybrel
safe but few potential drawbacks: more likely to have irregular and abnormal bleeding, pregnancy may remain undetected longer |
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Term
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Definition
1. implanon- 3 yr, single rod implant (etonogestrel)
2. Depo-Provera- medroxyprogesterone acetate-150mg in a suspension given IM, released over 3 mo, inhibit the release of gonadotropins, inhibition of FSH and LH+progestin effects on endometrium, problem with bleeding irregularities
3. progestin intrauterine (Mirena): levonorgestrel+IUD-20ug levonorgestrel released/day (up to 5 yr)
4. nuvaring-etonogestrel/ethinyl estradiol vaginal ring, rubber ring inserted into vagina monthly (removed after 3 weeks)
5. ortho-evra: norelgestromin/ethinyl estradiol transdermal patch |
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Term
| postcoital contraception- Yuzpe regimen |
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Definition
emergency contraception-"morning after pill"
1. Yupze regimen-high doses of estrogen taken within 72 hr after unprotected sexual intercourse-dose repeated 12 hr later
examples: Ovral Preven, LoOvral, Triphasil
mechanism of action: prevents ovulation, implantation
effectiveness: 75-90% reduction in pregnancies
problems: nausea, vomiting, effect on fetus in case of failure, mastalgia |
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Term
| postcoital contraception- progestin only |
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Definition
examples: Plan B, Ovrette
mechanism of action: prevents implantation
effectiveness: 89% reduction in pregnancies
problems: less nausea and vomiting than combinations |
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Term
| postcoital contraception- selective progesterone receptor modulator |
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Definition
| Ulipristal Acetate (ella) |
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Term
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Definition
Mifepristone (RU-486)
uses: postcoital contraceptive, abortifacient in combo with misoprostol (oral prostaglandin), can be used to ripen the cervix and induce labor
side effects: nausea, vomiting, pain, bleeding requiring medical intervention (5%) |
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Term
adverse effects of steroid contraceptives:
cardiovascular problems-estrogen dose dependent
the new combination OCs with lower estrogen content do not appear to increase CV disease risk unless other risk factors for CV exist |
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Definition
1. increased risk for myocardial infarction-estrogens do not cause atherosclerosis- but may increase the risk for the thrombotic event which results in occlusion of the coronary
risk factors: age, smoking, diabetes, hypertension, high LDL, low HDL
2. increased risk for cerebral vascular disease
3. increase in blood pressure- increased angiotensin synthesis
4. increased risk for thromboembolitic disorders (estrogen dose dependent; smoking and genetic factors (factor V Leiden) increase risk) |
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Term
| adverse effects with steroid contraceptives: effects on cancer risk |
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Definition
breast cancer- no significant difference
endometrial and ovarian cancer- decreased risk
cervical cancer- increased risk (not clinically verified), only risk seen after 5 years of use |
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Term
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Definition
gallbladder disease-may be a problem in women already at risk for GB disease
pregnancy-estrogens and progestins are pregnancy category X
increased rate of epiphyseal closure
decreased glucose tolerance-may occur due to progestin, a problem in women with diabetes |
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Term
| side effects of steroid contraceptives |
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Definition
1. nausea/vomiting
2. weight gain (changes in ACTH/aldosterone levels)
3. breast changes
4. acne, oily scalp (if compound has androgenic activity)
5. changes in menstrual flow- decrease in amount and duration, breakthrough bleeding-early to mid cycle- due to decreased estrogen, late cycle- due to decreased progestin, amenorrhea
6. changes in ocular contour |
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Term
| drug interactions-agents which may decrease the effectiveness of OC's |
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Definition
1. agents which increase metabolism of steroid OCs: barbiturates, hydantoins, rifampin, troglitazone, St Johns Wort
2. broad spectrum antibodies may increase OC failure |
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Term
| effect of OCs on the effectiveness of other drugs |
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Definition
decreases: warfarin, benzodiazepines-lorazepam, oxazepam
increases: tricyclic antidepressants, theophylline |
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Term
| therapeutic use of progestins |
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Definition
contraception
hormone replacement therapy (with estrogen)-clinical trial data seriously question this use
endometriosis- viable endometrial tissue in abnormal locations-contraceptives suppress FSH, LH release=endometrial atrophy, Danazol (Danocrine), GnRH agonists
disorders of menstrual bleeding- in combination OCs result in regular, lighter periods
acne-worsened by androgens, combination therapy will inhibit testosterone biosynthesis, Ortho-Tri-Cyclen approved for acne treatment |
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Term
| polycystic ovarian syndrome (PCOS) |
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Definition
hormone imbalance interferes with normal ovulation and other body systems. follicles develop but do not ovulate-swelling and fluid causes cyst formation
abnormal insulin production and metabolism may also affect the development of PCOS
symptoms: irregular menstrual cycles, androgenic effects on hair, skin, depression, or mood swings.
risks: reproductive (miscarriage, infertility, endometrial hyperplasia), metabolic (insulin, gestational diabetes, metabolic syndrome, type 2 diabetes, or obesity)
-cardiovascular (high blood pressure, coronary heart disease, high cholesterol)
treatments: reproductive strategy: combination oral contraceptives, metabolic strategy: metformin (Glucophage) |
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Term
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Definition
progesterone-micronized progesterone (prometrium)-oral or suppository
progesterone derivatives: medroxyprogesterone acetate (provera) 1st generation oral or IM injection. longer duration, hydroxyprogesterone caproate (Hylutin)-IM injection |
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Term
| megestrol acetate (megace) |
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Definition
used to stimulate appetite in AIDS and cancer patients
also: endometriosis, hot flashes, breast, prostate cancer |
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